Basic Information
ID: ALA1795261
Journal: Eur J Med Chem
Title: HIF-1α inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
Authors: Xia Y, Jin Y, Kaur N, Choi Y, Lee K.
Abstract: The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
CiteXplore: 21481991
DOI: 10.1016/j.ejmech.2011.03.022
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets